[F-18]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils

Abstract

In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for beta-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [I-125]TZDM against beta-amyloid 1-42 (A beta 42) aggregates. Two new [F-18]-labeled isoindole derivatives were synthesized and evaluated as potential beta-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [F-18]18b and [F-18]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of A beta fibrils in the brains of Alzheimer's disease (AD) patients. (C) 2008 Elsevier Ltd. All rights reserved.